产品
编 号:F741594
分子式:C23H24N6O3
分子量:432.48
产品类型
结构图
CAS No: 2438637-64-8
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产品详情
生物活性:
GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1), with mean Kiapp values of 21 nM, 189 nM and 691 nM for human mouse and rat RIP1, respectively.
体内研究:
GNE684 also had no impact on overall survival or tumor growth in the KPP or KPR (LSL-Kras G12D/+; p16/p19 fl/wt ; Trp53 R270H/wt ; Pdx1-cre) PDAC models.GNE684 (50mg/kg; p.o. twice daily) inhibits colitis and ileitis caused by NEMO deficiency in intestinal epithelial cells (IECs).Animal Model:Nemofl/fl Villin.creERT2 mice (NEMO IEC-KO)
Dosage:50 mg/kg
Administration:Oral administration; twice daily; from days 2–6 treated with tamoxifen
Result:Almost completely protected the NEMO-deficient intestines from colitis and ileitis.
体外研究:
GNE684 (20 μM; 20 hours) inhibits RIP1 kinase driven cell death effectively in several human and mouse cell lines.GNE684 (20 μM; 0-60 minutes) disrupts TBZ (2 μM BV6, 20 ng/ml TNF, 20 μM zVAD)-induced RIP1 autophosphorylation, interactions between RIP1 and RIP3, RIP3 autophosphorylation, and phosphorylation of MLKL by RIP3.